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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on the storage and integration of epigenetic drug datasets that were obtained from laboratory experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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GSK126

Category:HMTi
Cas Number:1346574-57-9
Molecular Formula:C31H38N6O2
Molecular Weight:526.67242 g/mol
Smiles:CCC(C)N1C=C(C2=C(C=C(C=C21)C3=CN=C(C=C3)N4CCNCC4)C(=O)NC
C5=C(C=C(NC5=O)C)C)C
Description:GSK126 induced a 50% loss of H3K27 tri-methylation (H3K27me3) in both EZH2 wild-type and mutant DLBCL cell lines at concentrations ranging from 7–252 nM independent of EZH2 mutation status. GSK126 suppresses cell proliferation of a panel of B-cell lymphoma cell lines. Six of the seven most sensitive DLBCL cell lines harboured Y641N, Y641F or A677G EZH2 mutations (growth IC50 = 28–861  nM). 72 h treatment with 500 nM GSK126 induces transcriptional activation in sensitive cell lines.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (9.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
1142 GSK126Monoamine oxidase (Homo sapiens (Human))25600407
1143 GSK126Dopamine receptor D2 and D3 (Rattus norvegicus (Rat))24848155
1144 GSK126LSD1/CoREST complex (Homo sapiens (Human))21382717
1145 GSK126LSD1/CoREST complex (Homo sapiens (Human))21596573
1146 GSK126Cytochrome P450 2B6 (Homo sapiens (Human))19049427
1147 GSK126Cytochrome P450 2C19 (Homo sapiens (human))19049427
1148 GSK126Cytochrome P450 2C19 (Homo sapiens (human))21189020
1149 GSK126Cytochrome P450 2B6 (Homo sapiens (Human))21189020
1150 GSK126Cytochrome P450 2C19 (Homo sapiens (human))21384875
1151 GSK126Cytochrome P450 2B6 (Homo sapiens (Human))21384875
1152 GSK126Monoamine oxidase (Homo sapiens (human))15537343
1153 GSK126Monoamine oxidase (Homo sapiens (Human))15027872
1154 GSK126trace amine-associated receptor 1 (Homo sapiens)
1155 GSK126guanine nucleotide-binding protein subunit alpha-15 (Homo sapiens)
1156 GSK126guanine nucleotide-binding protein subunit alpha-15 (Homo sapiens)
1157 GSK126race amine-associated receptor 1 (Homo sapiens)
1158 GSK126Lysine-specific histone demethylase 1B (Homo sapiens)24131029
1159 GSK126LSD1/CoREST complex (Homo sapiens (Human))24131029
1160 GSK126LSD1/CoREST complex (Homo sapiens (Human))24131029
1161 GSK126LSD1/CoREST complex (Homo sapiens (Human))24237195
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Disease list

ConditionsDrug NameStatusNct NumberPhases
ARID1A mutated OVISEGSK126Preclinical study
lymphoblastic leukemiaGSK126Preclinical study
lymphomaCPI360
EPZ-6438
GSK126
Preclinical study
DLBCLGSK126Preclinical study
healthyGSK126Preclinical study
healthyC646
GSK126
KDM5-C70
Preclinical study
healthyGSK343
GSK126
Preclinical study
adipose-derived mesenchymal (AMSCs)GSK126Preclinical study
colon carcinomaGSK126
Trichostatin A
Preclinical study
Primary ovarian cancerGSK126Preclinical study
peripherial mononuclearGSK126Preclinical study
DLBCLGSK126Preclinical study

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Targeting EZH2 methyltransferase activity in ARID1A mutated cells as a synthetic lethal therapeutic strategy GSK126HMTiARID1A mutated OVISE cells 25686104
A687V EZH2 is a driver of histone H3 lysine 27 (H3K27) hyper-trimethylation GSK126HMTihuman lymphoblastic leukemia cell lines (SUP-B8, NALM-6)25253781
EZH2 inhibitor efficacy in non-Hodgkin lymphoma does not require suppression of H3K27 mono-methylation CPI360
EPZ-6438
GSK126
HMTihuman lymphoma cell line(Karpas422)25457180
Gene expression profiling of EZH2 mutant and wild type DLBCL cell lines treated with EZH2 inhibitor GSK126HMTihuman DLBCL cell lines (Pfeiffer, KARPAS-422, WSU-DLCL2, SU-DHL-10, SU-DHL-6, DB , SU-DHL-4. HT, OCI-LY-19 and Toledo)23051747
Inhibition of EZH2 in THP-1 cells GSK126HMTihuman THP-1 cell line
A multiplexed system for quantitative comparisons of chromatin landscapes C646
GSK126
KDM5-C70
HATi
HMTi
KDMi
K562 cells SKM-1 and Toledo cells Human HSCs 26687680
PRC2 inhibition counteracts the culture-associated loss of engraftment potential of human cord blood-derived hematopoietic stem and progenitor cells GSK343
GSK126
HMTiCord blood hematopoietic stem cells (CB-HSCs)26198814
Epigenetic Control of Skeletal Development by the Histone Methyltransferase Ezh2 GSK126 HMTihuman adipose-derived mesenchymal (AMSCs)?26424790
Finding missing proteins from epigenetically manipulated human cells GSK126
Trichostatin A
HMTi
HDACi
A549; HCT116 and MHCC97H cells26202631
Epigenetic silencing of Th1 chemokines shapes tumor immunity, immunotherapy and patient outcome [GSK126] GSK126HMTiPrimary ovarian cancer cells26503055
Expression data from monocytes and monocyte derived macrophages GSK126HMTihuman peripherial mononuclear cells
ChIP-seq analysis of H3K27me3 histone modification in EZH2 mutant and wild type DLBCL cell lines GSK126HMTiEZH2 mutant and wild type DLBCL cell lines23051747

Complex list

PDBIdDrug NameTargetmethodPubmedId

About

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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on integrating epigenetic drug studies based Omics data from high through experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

Copyright

©2016 Group of Computational Epigenomics and Bioinformatics, College of Life Science, Jilin Normal University, China

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